P
US9937171B2ActiveUtilityPatentIndex 47

Methods of blocking the CXCR-4/SDF-1 signaling pathway with inhibitors of bruton's tyrosine kinase

Assignee: ACERTA PHARMA BVPriority: Apr 11, 2014Filed: Apr 10, 2015Granted: Apr 10, 2018
Est. expiryApr 11, 2034(~7.8 yrs left)· nominal 20-yr term from priority
Inventors:IZUMI RAQUELSALVA FRANCISCOHAMDY AHMED
A61K 31/454A61K 31/52A61K 31/4985A61K 31/519
47
PatentIndex Score
0
Cited by
80
References
17
Claims

Abstract

In some embodiments, the present invention relates to novel small molecule inhibitors that block the CXCR4-SDF-1 signaling pathway by directly inhibiting members of the Tec family of kinases, namely Bruton's tyrosine kinase (BTK), and their use in treating diseases in which pathogenesis is mediated by the CXCR4/SDF-1 signaling pathway.

Claims

exact text as granted — not AI-modified
We claim: 
     
       1. A method of treating nephropathy in a human subject having overexpression of CXCR4, comprising (i) measuring CXCR-4 expression in a tissue sample isolated from the human subject, and (ii) administering to the human subject a pharmaceutical composition comprising an amount of a compound of the formula: 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof effective to reduce expression of CXCR-4. 
     
     
       2. The method of  claim 1 , wherein the nephropathy is IgA nephropathy. 
     
     
       3. The method of  claim 1 , wherein the nephropathy is membranous nephropathy. 
     
     
       4. The method of  claim 1 , wherein the measuring CXCR-4 expression is done before administration of the pharmaceutical composition. 
     
     
       5. The method of  claim 1 , wherein the measuring CXCR-4 expression is done after administration of the composition. 
     
     
       6. The method of  claim 4  or  5 , wherein the CXCR-4 expression is measured on peripheral blood mononuclear cells isolated from the blood of the human subject. 
     
     
       7. The method of  claim 1 , wherein the pharmaceutical composition is administered orally. 
     
     
       8. The method of  claim 7 , wherein the pharmaceutical composition is formulated as a capsule. 
     
     
       9. The method of  claim 8 , wherein the capsule is a gelatin capsule. 
     
     
       10. The method of  claim 8 , wherein the capsule contains about 140 mg of the compound. 
     
     
       11. The method of  claim 1 , wherein the amount of the compound effective to reduce CXCR-4 expression is about 1 mg to about 500 mg daily. 
     
     
       12. The method of  claim 1 , wherein the amount of the compound effective to reduce CXCR-4 expression is about 10 mg to about 300 mg daily. 
     
     
       13. The method of  claim 1 , wherein the amount of the compound effective to reduce CXCR-4 expression is about 20 mg to about 250 mg daily. 
     
     
       14. The method of  claim 1 , wherein the amount of the compound effective to reduce CXCR-4 expression is about 10 mg to about 200 mg daily. 
     
     
       15. The method of  claim 1 , wherein the amount of the compound effective to reduce CXCR-4 expression is about 20 mg to about 150 mg daily. 
     
     
       16. The method of  claim 1 , wherein the pharmaceutical composition comprises a compound of the formula: 
       
         
           
           
               
               
           
         
       
     
     
       17. The method of  claim 1 , wherein the pharmaceutical composition comprises a pharmaceutically acceptable salt of the compound of the formula:

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